Somatostatin (srif); Related Peptides Patents (Class 530/311)
  • Patent number: 4798821
    Abstract: Process and compositions for lowering blood pressure in diabetic by employing a cyclopeptide compound is described.
    Type: Grant
    Filed: March 2, 1987
    Date of Patent: January 17, 1989
    Assignee: Merck & Co., Inc.
    Inventor: John F. Hartmann
  • Patent number: 4728638
    Abstract: Somatostatine derivatives of the general formula ##STR1## wherein either (a)A is ##STR2## W is -CO-N(A.sub.4) or -N(A.sub.5)-CO- and Y.sub.1 and Y.sub.2 are H or together a bondor (b)A is H, alkyl, phenylalkyl or RCO andY.sub.1 and Y.sub.2 are acyl groups as defined in claim 1,A', B, C, D, E, F, A.sub.1, A.sub.2, A.sub.3, A.sub.4, A.sub.5, R and Z having the meanings recited in claim 1, have pharmacological, in particular GH-, gastric- and pancreatic secretion inhibiting activity.
    Type: Grant
    Filed: January 7, 1986
    Date of Patent: March 1, 1988
    Assignee: Sandoz Ltd.
    Inventors: Wilfried Bauer, Janos Pless, Rene Huguenin
  • Patent number: 4703034
    Abstract: There is disclosed a series of novel cyclic tetrapeptides related to somatostatin. The compounds have surprisingly been found to have the activity of increasing blood glucose when administered. The compounds are prepared using the solid phase or mixed anhydride synthesis methods and compositions and methods utilizing the novel compounds are also disclosed.
    Type: Grant
    Filed: April 28, 1986
    Date of Patent: October 27, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Roger Freidinger, Ruth F. Nutt, Terry A. Lyle, Richard Saperstein
  • Patent number: 4663435
    Abstract: Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a bridged grouping which replaces eight of the ring amino acids of somatostatin. The bridged cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of selectively inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These bridged cyclic hexapeptides are prepared by the solid phase method.
    Type: Grant
    Filed: June 24, 1985
    Date of Patent: May 5, 1987
    Assignee: Merck & Co., Inc.
    Inventor: Stephen F. Brady
  • Patent number: 4650787
    Abstract: Novel compositions of the formula ##STR1## wherein A represents an L, D or DL amino-acid selected from the group consisting of Ala, Val, Phe, p-Cl-Phe, Trp, Pro, Ser, Thr, Glu, Gly, Beta Ala, Abu, N-Me Ala, 5-F-Trp, 5-Br-Trp, 5-Cl-Trp, their acetylated derivatives or a pharmaceutically acceptable acid addition salt thereof;B represents an L, D or DL amino acid amide selected from the group consisting of Thr NH.sub.2, Val NH.sub.2, Pro NH.sub.2, HO-Pro NH.sub.2, Ser NH.sub.2, Tyr NH.sub.2, Trp NH.sub.2, 5-F-Trp NH.sub.2, For-Trp NH.sub.2, Ala NH.sub.2, Gly NH.sub.2, Me Ala NH.sub.2 ;X represents L-Phe or L-Tyr,Y represents L-Thr or L-Val;Z is L, D or DL-5-F-Trp, 5-Br-Trp, 5-Cl-Trp, 5-I-Trp or D-Trp; andC" and C' represent L or D Cys, Abu, Asp or Lys; and the pharmaceutically acceptable acid addition salts thereof; are useful as agents for inhibiting the release of growth hormone, for the treatment of gastrointestinal disorders and for therapy of certain cancers and the management of diabetes.
    Type: Grant
    Filed: April 25, 1985
    Date of Patent: March 17, 1987
    Inventors: Andrew V. Schally, Ren Z. Cai
  • Patent number: 4623716
    Abstract: Peptides, such as calcitonin, having two cysteine residues connected by a disulfide bond are prepared by a process which includes the step of cyclizing the cysteines at a pH of 8.5 to 9.0, and a concentration of 0.4 to 1.8 mg of peptide per ml of solution. These novel conditions produce rapid cyclization with an unforeseen improvement in yield.
    Type: Grant
    Filed: November 1, 1984
    Date of Patent: November 18, 1986
    Assignee: USV Pharmaceutical Corp.
    Inventors: David Stevenson, Mohammad A. Islam
  • Patent number: 4621073
    Abstract: The invention relates to cyclic hexapeptides of the general formula III ##STR1## in which X represents the radical of an L-aminoacid of the general formula IIIa ##STR2## in which A and B are identical or different and denote alkyl having 1 to 3 carbon atoms, or A and B together represent a saturated, unsaturated or aromatic monocyclic or bicyclic structure having 3 to 6 carbon atoms, n denotes 0 or 1, and Y represents an aliphatic or aromatic L-aminoacid the side chain of which can be hydroxylated, and their salts with physiologically tolerated acids, and to a process for their preparation and their use and their intermediates.
    Type: Grant
    Filed: January 31, 1984
    Date of Patent: November 4, 1986
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Axel Friedrich, Wolfgang Konig, Volker Teetz, Rolf Geiger, Jurgen K. Sandow
  • Patent number: 4612302
    Abstract: A method of increasing the clearance of particles from the blood stream of a vertebrate, which comprises administering to a vertebrate having a surplus of particles in the blood stream of the vertebrate an amount of a somatostatin analogue sufficient to increase phagocytosis in the vertebrate is disclosed along with a method treating vascular lesions or deterioration of biological membranes comprising the step of administering to a human or other mammal suspected of having one or more vascular lesions or of having deterioration of a biological membrane in the liver of said human or mammal an amount of a somatostatin analogue sufficient to reduce the number or severity of said lesions or to prevent further deterioration or reduce the extent of deterioration of said membrane.
    Type: Grant
    Filed: November 14, 1983
    Date of Patent: September 16, 1986
    Assignee: Brigham and Women's Hospital
    Inventors: Sandor Szabo, Klaus W. Usadel, Horst Kessler
  • Patent number: 4612366
    Abstract: Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a secondary amino acid which replaces seven of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method and/or solution synthesis.
    Type: Grant
    Filed: June 17, 1985
    Date of Patent: September 16, 1986
    Assignee: Merck & Co., Inc.
    Inventor: Ruth F. Nutt
  • Patent number: 4611054
    Abstract: Cyclic hexapeptide somatostatin analogs are prepared wherein a peptide surrogate replaces eight of the ring amino acids of somatostatin. The cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These cyclic hexapeptides are prepared by the solid phase method.
    Type: Grant
    Filed: April 29, 1985
    Date of Patent: September 9, 1986
    Assignee: Merck & Co., Inc.
    Inventor: Roger Freidinger